反应详情

To a solution of triphenylphosphine (2 eq) in THF was added di-terbutylazodicarboxylate (2 eq). The mixture was stirred 15 minutes at ambient temperature under nitrogen atmosphere. To that was added tert.butyl-4-hydroxypiperidine-1-carboxylate (5 eq). The mixture was stirred 15 minutes at ambient temperature followed by addition of 5-bromo-2-chloroquinazolin-8-ol (1 eq). The mixture was stirred overnight at ambient temperature. The reaction mixture was concentrated and the residue was purified by flash column chromatography (25% EtOAc/Hexane) to provide product as a white solid in 90% yield. ES/MS m/z 442.1 (MH+).

1. stirringThe mixture was stirred 15 minutes at ambient temperature
2. stirringThe mixture was stirred overnight at ambient temperature
3. concentrationThe reaction mixture was concentrated
4. customthe residue was purified by flash column chromatography (25% EtOAc/Hexane)
5. customto provide product as a white solid in 90% yield